Abstract
Bioassay-guided fractionation of the acetone extract of the roots of Casearia membranacea furnished three new clerodane diterpenes, caseamembrins S-U (1-3) and the known caseamembrin Q (4). Their structures were established by extensive spectroscopic analyses, especially 2D-NMR. Compounds 1-4 were tested against human tumor cells, including HeLa (cervical epitheloid carcinoma), DLD-1 (colon carcinoma), Daoy (medulloblastoma), and KB (oral epidermoid carcinoma) cell lines. Caseamembrin T (2) exhibited the most potent activity against Daoy cells (ED(50)=10 ng/ml), superior to that of the standard drug mitomycin.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / isolation & purification
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Antineoplastic Agents / pharmacology*
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Casearia / chemistry*
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Diterpenes, Clerodane / chemistry*
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Diterpenes, Clerodane / isolation & purification
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Diterpenes, Clerodane / pharmacology*
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Drug Screening Assays, Antitumor
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HeLa Cells
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Humans
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Magnetic Resonance Spectroscopy / methods
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Magnetic Resonance Spectroscopy / standards
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Molecular Conformation
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Plant Roots / chemistry*
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Reference Standards
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Diterpenes, Clerodane